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lopinavir + ritonavir or darunavir + ritonavir
- Development stage
- Unknown
- Lead developer
- ANRS
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
This refers to the boosted protease inhibitor regimens used in the ANRS 12286 (MOBIDIP) Phase III clinical trial. The regimen consists of either lopinavir/ritonavir (200/50 mg) or darunavir/ritonavir (800/100 mg). These are small molecule HIV-1 protease inhibitors. Lopinavir and darunavir inhibit the cleavage of Gag-Pol polyproteins, preventing the formation of mature, infectious virus particles. Ritonavir is used as a pharmacokinetic enhancer (booster) to inhibit the CYP3A4 enzyme, thereby increasing the plasma concentrations of the primary protease inhibitor. The MOBIDIP trial evaluated these boosted PIs as monotherapy versus dual therapy with lamivudine for maintenance in virologically suppressed HIV-1 patients on second-line treatment in Africa.
- Brand names
- KaletraAluviaPrezistaNorvir
- Other names
- boosted lopinavirboosted darunavirLPV/rDRV/rboosted protease inhibitorsPI/r
02
Targets
CYP3A4 (Cytochrome P450 3A4)PR (Progesterone receptor)
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